Home > Products > Neuronal Signaling > Beta Amyloid > DAPT

DAPT

(CAS No:208255-80-5)

DAPT (GSI-IX) is a novel γ-secretase inhibitor, which inhibits Aβ production with IC50 of 20 nM in HEK 293 cells.

CAS No:208255-80-5

Molecular Weight(MW):432.46

Purity:98%+

Specification:500mg;1g;5g;10g;50g;100g

Price and large packaging, please e-mail consultation:info@SuperLan-chem.com

QC Documents

COA	MSDS	HPLC	NMR

ChemicalInfomation

CAS No:	208255-80-5
Molecular formula(MF)	C₂₃H₂₆F₂N₂O₄
Molecular Weight(MW):	432.46
Alias

Solubility

In vitro	DMSO	86 mg/mL (198.86 mM)
	Ethanol	50 mg/mL (115.61 mM)
	Water	<1 mg/mL
In vivo	4% DMSO+corn oil	10mg/mL

Biological Activity

Description

DAPT (GSI-IX) is a novel γ-secretase inhibitor, which inhibits Aβ production with IC50 of 20 nM in HEK 293 cells.

Targets

γ secretase(Aβ) ^[1]
(HEK 293 cells)

20 nM

In vitro

In human primary neuronal cultures, DAPT also shows inhibitory effects on Aβ production with IC50 of 115 nM and 200 nM respectively for Aβ total and Aβ42, which is 5-10-fold lower than is observed in HEK 293 cells. ^[1] A recent study shows that DAPT inhibits the proliferation of SK-MES-1 cells in a concentration-dependent manner with IC50 of 11.3 μM. In addition, DAPT also induces caspase-dependent and caspase-independent apoptosis in lung squamous cell carcinoma cells by inhibiting Notch receptor signaling pathway. ^[2]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
A549 CD133−	Growth Inhibition Assay	2 Î¼M	48 h		enhances cell growth inhibition induced by CDDP	24502949
A549 CD133+	Growth Inhibition Assay	2 Î¼M	48 h		enhances cell growth inhibition induced by CDDP	24502949
HT29	Growth Inhibition Assay	0.5-75 Î¼M	12/24/48 h	DMSO	inhibits the cell growth in a concentration manner	25257945
SHG-44	Growth Inhibition Assay	0.5-10 Î¼M	1-5 d		inhibits the cell viability at the optimal concentration of 1 Î¼M	25063285
MG63	Function Assay	100 Î¼M	24 h	DMSO	desensitizes the cell line to cisplatin treatment	24894297
Saos-2	Function Assay	100 Î¼M	24 h	DMSO	desensitizes the cell line to cisplatin treatment	24894297
U251	Growth Inhibition Assay	2 Î¼M	48 h	DMSO	strengthensÂ t-AUCB-induced cell growth suppression	24793313
U87	Growth Inhibition Assay	2 Î¼M	48 h	DMSO	strengthensÂ t-AUCB-induced cell growth suppression	24793313
U251	Function Assay	2 Î¼M	48 h	DMSO	blocksÂ t-AUCB-induced activation of the p38 MAPK/MAPKAPK2/Hsp27 pathway and inhibits expression of NICD1	24793313
U87	Function Assay	2 Î¼M	48 h	DMSO	blocksÂ t-AUCB-induced activation of the p38 MAPK/MAPKAPK2/Hsp27 pathway and inhibits expression of NICD1	24793313
A549	Growth Inhibition Assay	10 Î¼M	24h		decreases the cell viability combined with PTE	23671619
GC-B	Growth Inhibition Assay	6.25-100 Î¼M	24 h	DMSO	inhibits the cell growth in a dose-dependent manner	19542446

... Click to View More Cell Line Experimental Data

In vivo

DAPT administration (100mg/kg) leads to a robust and sustained pharmacodynamic effect in PDAPP mice that DAPT levels in the brain exceeds 100 ng/g within 1 hour and persists up to 18 hours after administration, with peak levels of 490 ng/g observed after 3 hour. And during the period, DAPT (100 mg/kg) also reduces the cortical total Aβ and Aβ42 in a dose-dependent manner with a 50% reduction. ^[1] In rat cerebral cortexes, DAPT (40 mg/kg) suppresses the LPS-induced activity of γ-secretase and increases the cell apoptosis with the prolonged neuroinflammation. ^[3]